Tag: M.W=100-150

Ramil, Carlo P. published the artcileSequence-Specific 2-Cyanobenzothiazole Ligation, HPLC of Formula: 133627-45-9, the main research area is cyanobenzothiazole ligation protein labeling.

The use of small, natural chem. reporters in conjunction with catalyst-free bioorthogonal reactions will greatly streamline protein labeling in a cellular environment with min. perturbation to their function. Here we report the discovery of a 2-cyanobenzothiazole (CBT)-reactive peptide tag, CX10R7, from a cysteine-encoded peptide phage library using the phage-assisted interrogation of reactivity method. Fusion of CX10R7 with a protein of interest allows site-specific labeling of the protein with CBT both in vitro and on the surface of E. coli cells. Mutagenesis studies indicated that the reactivity and specificity of CX10R7 are attributed to the sequence environment, in which the residues surrounding cysteine help to stabilize the ligation product.

Journal of the American Chemical Society published new progress about Aromatic nitriles Role: RCT (Reactant), RACT (Reactant or Reagent). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, HPLC of Formula: 133627-45-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Huiping published the artcileSynthesis of 2-cyanoacrylates containing pyridinyl moiety under ultrasound irradiation, COA of Formula: C6H7ClN2, the main research area is pyridinylaminocyanoacrylate preparation antitumor; cyanoacrylate pyridinylamino preparation antitumor; methylthiocyanoacrylate pyridinamine substitution ultrasound.

Reaction of NCCH2CO2Et with CS2 and Me2SO4 in the presence of NaOMe in anhydrous MeOH yields 2-cyano-3,3-bis(methylthio)acrylate. Further nucleophilic substitution with 3-amino-2-chloro-4-methylpyridine under ultrasonic irradiation afforded 3-[(2-chloro-4-methylpyridin-3-yl)amino]-2-cyano-3-methylthioacrylate as key intermediate. The title compounds were then obtained through the reaction of the key intermediate with primary aliphatic amines under reflux. All new structures were verified by elemental anal., IR, 1H NMR and mass spectra. In the MTT test, the compounds were found to possess moderate antitumor activities against PC3 and A431 cells.

Journal of Heterocyclic Chemistry published new progress about Aliphatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, COA of Formula: C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Savarimuthu, Sebastian Antony published the artcileDBU-Mediated Intermolecular 5-exo-dig Cyclization of Propargyl Alcohols and Carbon Disulfide to [1,3]-Oxathiole-2-thiones, Computed Properties of 71255-09-9, the main research area is propargyl alc preparation carbon disulfide DBU regioselective cyclization; aryl oxathiole thione preparation.

A novel metal-free method was proposed to produce [1,3]-oxathiole-2-thiones from a readily synthesized propargyl alcs. and easily accessible carbon disulfide, where both secondary and primary propargyl alcs. were compatible to this methodol. This procedure was simple, versatile, atom economy and functional group tolerance resulting in moderate to excellent yields. Finally, the process was screened on different mode of reaction operation.

ChemistrySelect published new progress about Alkynyl alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hu, Min-Qi published the artcileA one-pot approach to construct 3-(2-methoxypyridin-3-yl)-4H-chromen-4-ones via meinwald rearrangement/intramolecular demethylation annulation of epoxides, Application In Synthesis of 71255-09-9, the main research area is methoxypyridinyloxiranyl methoxyphenylmethanone tandem one pot Meinwald demethylation heterocyclization; methoxypyridinyl chromenone preparation phenylboronic acid palladium catalyst Suzuki coupling; phenyl methoxypyridinyl chromenone preparation.

A convenient and practical approach for construction of 3-(2-methoxypyridin-3-yl)-4H-chromen-4-ones was successfully developed by a one-pot Meinwald rearrangement/intramol. demethylation/annulation reaction sequence with easily accessible epoxides as the starting material. The synthetic protocol was of excellent functional group compatibility under mild reaction conditions, and 3-(2-methoxypyridin-3-yl)-4H-chromen-4-ones were obtained in high yields. Moreover, further derivation successfully furnished more complicated derivatives by Suzuki-Miyaura cross-coupling reaction which may provide a promising potential application in exploring biol. activity of 3-aryl-4H-chromen-4-ones.

Heterocycles published new progress about Demethylation. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application In Synthesis of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Choi, Ji Won published the artcileOptimization of vinyl sulfone derivatives as potent nuclear factor erythroid 2-related factor 2 (Nrf2) activators for Parkinson’s disease therapy, Computed Properties of 71255-09-9, the main research area is vinyl sulfone derivative Nrf2 activator Parkinson disease therapy.

We previously developed a novel series of vinyl sulfones as nuclear factor erythroid 2-related factor 2 (Nrf2) activators with therapeutic potential for Parkinson’s disease (PD). However, the previously developed lead compound (1) exhibited undesirable druglike properties. Here, we optimized vinyl sulfones by introducing nitrogen heterocycles to improve druglike properties. Among the synthesized compounds, 17e was the most promising drug candidate with good druglike properties. Compound 17e showed superior effects on Nrf2 activation in cell-based assays compared to compound 1 (17e: half-maximal effective concentration (EC50) = 346 nM; 1: EC50 = 530 nM). Compound 17e was further confirmed to induce expression of Nrf2-dependent antioxidant enzymes at both mRNA and protein levels. In a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse model of PD, 17e significantly attenuated loss of tyrosine hydroxylase-immunopos. dopaminergic neurons, suppressed microglial activation, and alleviated PD-associated motor dysfunction. Thus, 17e is a novel Nrf2 activator with excellent druglike properties and represents a potential therapeutic candidate for PD.

Journal of Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (HO-1, expression induction). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Choi, Peter J. published the artcileSynthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units, HPLC of Formula: 71255-09-9, the main research area is bedaquiline analog antituberculosis thiophene furan pyridine; mol structure biol activity; Bedaquiline; Bedaquiline analogues; Drug development; Tuberculosis.

Analogs of bedaquiline (I) where the Ph B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesized and evaluated. While there was an expected broad pos. correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an addnl. contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and showed acceptable oral bioavailability, but there was only limited (and unpredictable) improvement in their hERG liability.

Bioorganic & Medicinal Chemistry Letters published new progress about Pyridines Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, HPLC of Formula: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Vu, Hoang Nam published the artcileSynthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists, Product Details of C6H7ClN2, the main research area is thiazolecarboxamide aryl preparation metabotropic glutamate receptor antagonist; picolinamide aryl preparation metabotropic glutamate receptor antagonist; Antagonist; Metabotropic glutamate receptor; Molecular docking; Picolinamides; Thiazole-2-carboxamides.

Herein the synthesis and biol. evaluation of picolinamides and thiazole-2-carboxamides as potential mGluR5 antagonists are described. It was found that a series of N-aryl-4-R-2-thiazolecarboxamides (R = Br, Me, CN; aryl = 3-FC6H4, 3-NCC6H4, 2-pyridyl, 6-chloro-2-pyridyl, etc.) (I) showed better inhibitory activity against mGluR5. The compounds I (R = Br; aryl = 3-BrC6H4, 6-methyl-2-pyridyl) have been identified as potent antagonists (IC50 = 274 and 159 nM) showing excellent in vitro stability profile. Mol. docking study using the crystal structure of mGluR5 revealed that these two compounds fit the allosteric binding site of mavoglurant well.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Product Details of C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Huan published the artcileSynthesis and Evaluation of 1,2,4-Triazolo[1,5-a]pyrimidines as Antibacterial Agents Against Enterococcus faecium, Product Details of C7H7NO2, the main research area is vancomycin resistant Enterococcus faecium infection antibacterial triazolopyrimidine; triazolopyrimidine preparation metabolic stability low intrinsic clearance; cell wall biosynthesis antibiotic target triazolopyrimidine; aldehyde three component Biginelli heterocyclization dicarbonyl compound alkylthiotriazolamine.

Rapid emergence of antibiotic resistance is one of the most challenging global public health concerns. In particular, vancomycin-resistant Enterococcus faecium infections have been increasing in frequency, representing 25% of enterococci infections in intensive care units. A novel class of 1,2,4-triazolo[1,5-a]pyrimidines, e.g., I [R1 = C6H4R’, 2-thienyl, 3-thienyl, 2-furyl, 2-pyrrolyl, 2-imiazolyl, 3-indolyl, 3-pyridyl, 2-methoxy-3-pyridyl, 4-pyridyl, cyclohexyl; R’ = i-Pr-4, H, Me-4, Et-4, i-Bu-4, OH-4, OMe-4, OH-3-OMe-4, (OMe)2-3,4, O(Pr-i)-4, OCF3-4, SMe-4, etc.], II [R1 = C6H4NMe2-4, R2 = OEt,NHMe, R3 = SCH2Ph; R1 = 2-thienyl, R2 = OEt, R3 = SCH2C6H4CO2H-4], III [R1 = C6H4NMe2-4, R3 = SCH2Ph; R1 = C6H4OMe-4, C6H4OEt-2, R3 = SCH2C6H4CO2H-4; R1 = C6H3(OMe)2-3,4, R3 = CH2C6H4F-4; R1 = C6H4Cl-4, R3 = SCH2-(2-naphthyl)],. IV [R1 = C6H4NMe2-4, R2 = H, R3 = SCH2Ph; R1 = C6H4Me-4, R2 = H, R3 = SCH2C6H4Me-2; R1 = C6H4Me-4, R2 = Me-2, Me2-2,4, R3 = SCH2C6H4Me-3; R1 = C6H4Et-4, R2 = H, Me-2, R3 = SCH2C6H4OMe-3; etc.], V [R3 = H, NH2, CO2Me, CO2Et, SMe, SCH2CONH2, SCH2CO2Et, SCH2CH2NHCO2CH2Ph, SCH2-(4-pyridyl), S(2-pyridyl), SCH2C6H4R”-4; R” = Me, OMe, SMe, CF3, OCF3, SCF3, NO2, CN, CO2H, CO2Me] and VI [R1 = 2-thienyl, R3 = H; R1 = C6H4CHMe2-4, C6H4CO2H-4, R3 = SCH2CH2NHCO2CH2Ph], active against E. faecium is reported herein. We used a three-component Biginelli-like heterocyclization reaction for the synthesis of a series of these derivatives based on reactions of aldehydes, β-dicarbonyl compounds, and 3-alkylthio-5-amino-1,2,4-triazoles. The resulting compounds were assayed for antimicrobial activity against the ESKAPE panel of bacteria, followed by investigation of their in vitro activities. These analyses identified a subset of 1,2,4-triazolo[1,5-a]pyrimidines that had good narrow-spectrum antibacterial activity against E. faecium and exhibited metabolic stability with low intrinsic clearance. Macromol. synthesis assays revealed cell-wall biosynthesis as the target of these antibiotics.

Journal of Medicinal Chemistry published new progress about Acinetobacter baumannii (antimicrobials). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Product Details of C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Yue-Mei published the artcileSyntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs), Recommanded Product: 2-Methoxynicotinaldehyde, the main research area is heterocyclic arylsulfone derivative preparation matrix metalloproteinase inhibitor.

Several classes of arylsulfone-based MMP-2/-9 inhibitors utilizing 6- to 8-membered heterocyclic rings, e.g., I, as zinc-binding groups (ZBGs) have been synthesized and their enzyme inhibitory activities were evaluated. Although a number of 6- and 7-membered heterocycles were effective, the most potent arylsulfone inhibitors are based on the rigid 1- or 3-hydroxypyridone ZBG.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship, metalloproteinase-inhibiting. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Recommanded Product: 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Annamalai, Murali published the artcileHighly stereoselective synthesis of a compound collection based on the bicyclic scaffolds of natural products, Name: 2-Methoxynicotinaldehyde, the main research area is bicyclic compound diastereoselective preparation lipophilicity; Aza-heterocycles; European Lead Factory; drug discovery; natural products; scaffolds.

A natural product inspired synthesis of six different chemotypes and their derivatives for drug discovery research was reported. These bicyclic hetero- and carbocyclic scaffolds are highly novel, rich in sp3 features and with ideal physicochem. properties to display drug likeness. The functional groups on the scaffolds were exploited further to generate corresponding compound collections. Synthesis of two of these collections exemplified with ca. 350 compounds are each also presented. The whole compound library is being exposed to various biol. screenings within the European Lead Factory consortium.

Molecules published new progress about Diastereoselective synthesis. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Name: 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem